Criteria for the design and biological characterization of radiolabeled peptide-based pharmaceuticals(557 views) Benedetti E, Morelli G, Accardo A, Mansi R, Tesauro D, Aloj L
Keywords: G Protein Coupled Receptor, Peptide, Radiopharmaceutical Agent, Animal Model, Cancer Diagnosis, Diagnostic Imaging, Drug Design, Drug Formulation, Human, Human Cell, In Vitro Study, In Vivo Study, Isotope Labeling, Mouse, Nonhuman, Priority Journal, Protein Expression, Review, Synthesis, Drug Evaluation, Preclinical, Italy, Biological,
Affiliations: *** IBB - CNR ***
CIRPeB, Dipartimento di Chimica Biologica, Università Federico II, Naples, Italy
Medicina Nucleare, Ist. Naz. Stud./Cura Tumori, Fondazione G. Pascale, Naples, Italy
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Dillman, R. O., Radiolabeled anti-CD20 monoclonal antibodies for the treatment of B-cell lymphoma (2002) J Clin Oncol, 20, pp. 3545-3557
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Behr, T. M., Jenner, N., Radetzky, S., Targeting of cholecystokinin-B/gastrin receptors in vivo: Preclinical and initial clinical evaluation of the diagnostic and therapeutic potential of radiolabelled gastrin (1998) Eur J Nucl Med, 25, pp. 424-430
Breeman, W. A., De Jong, M., Erion, J. L., Preclinical comparison of (111) Inlabeled DTPA- or DOTA-bombesin analogs for receptor-targeted scintigraphy and radionuclide therapy (2002) J Nucl Med, 43, pp. 1650-1656
Behr, T. M., Gotthardt, M., Earth, A., Imaging tumors with peptide-based radioligands (2001) Q J Nucl Med, 45, pp. 189-200
Mierke, D. F., Giragossian, C., Peptide hormone binding to G-protein-coupled receptors: Structural characterization via NMR techniques (2001) Med Res Rev, 21, pp. 450-471
Hamm, H. E., The many faces of G protein signaling (1998) J Biol Chem, 273, pp. 669-672
Bourne, H. R., How receptors talk to trimeric G proteins (1997) Curr Opin Cell Biol, 9, pp. 134-142
Baldwin, J. M., The probable arrangement of the helices in G protein-coupled receptors (1993) EMBO J, 12, pp. 1693-1703
Schwartz, M. A., Schaller, M. D., Ginsberg, M. H., Integrins: Emerging paradigms of signal transduction (1995) Annu Rev Cell Dev Biol, 11, pp. 549-599
Marshall, G. R., Peptide interactions with G-protein coupled receptors (2001) Biopolymers, 60, pp. 246-277
Wank, S. A., Cholecystokinin receptors (1995) Am J Physiol, 269, pp. G628-G646
Ji, Z., Hadac, E. M., Henne, R. M., Direct identification of a distinct site of interaction between the carboxyl-terminal residue of cholecystokinin and the type A cholecystokinin receptor using photoaffinity labeling (1997) J Biol Chem, 272, pp. 24393-24401
Anderson, C. J., Pajeau, T. S., Edwards, E. B., In vitro and in vivo evaluation of Copper-64-Octreotide conjugates (1995) J Nucl Med, 36, pp. 2315-2325
Baidoo, K. E., Scheffel, U., Stathis, M., High-affinity no-carrier-added 99mTc-labeled chemotactic peptides for studies of inflammation in vivo (1998) Bioconjug Chem, 9, pp. 208-217
Hnatowich, D. J., Qu, T., Chang, F., Labeling peptides with technetium-99m using a bifunctional chelator of a N-hydroxysuccinimide ester of mercaptoacetyltriglycine (1998) J Nucl Med, 39, pp. 56-64
Schwartz, D. A., Abrams, M. J., Hauser, M. M., Preparation of hydrazino-modified proteins and their use for the synthesis of technetium-99m-protein conjugates (1991) Bioconjug Chem, 2, pp. 333-336
Visser, G. W. M., Gerretsen, M., Herscheid, J. D. M., Labeling of monoclonal antibodies with rhenium-186 using the MAG3 chelate for radioimmunotherapy of cancer: A technical protocol (1993) J Nucl Med, 34, pp. 1953-1963
Friesner, R. A., Gunn, J. R., Computational studies of protein folding (1996) Annu Rev Biophys Biomol Struct, 25, pp. 315-342
Van Gunsteren, W. F., Berendsen, H. J., Molecular dynamics: Perspective for complex systems (1982) Biochem Soc Trans, 10, pp. 301-305
McCammon, J. A., Gelin, B. R., Karplus, M., Dynamics of folded proteins (1977) Nature, 267, pp. 585-590
Wu, R. S., Novel bifunctional linkers for antibody chelation with radiometals (1990) Cancer Treat Res, 51, pp. 215-232
Deshpande, S. V., Subramanian, R., McCall, M. J., Metabolism of indium chelates attached to monoclonal antibody: Minimal transchelation of indium from benzyl-EDTA chelate in vivo (1990) J Nucl Med, 31, pp. 218-224
Wank, S. A., G protein-coupled receptors in gastrointestinal physiology: I. CCK receptors: An exemplary family (1998) Am J Physiol, 274, pp. G607-G613
Berkner, K. L., Development of adenovirus vectors for the expression of heterologous genes (1988) Biotechniques, 6, pp. 616-629
Munson, P. J., LIGAND: A computerized analysis of ligand binding data (1983) Methods Enzymol, 92, pp. 543-576
Rovati, G. E., Rodbard, D., Munson, P. J., DESIGN: Computerized optimization of experimental design for estimating Kd and Bmax in ligand binding experiments: II. Simultaneous analysis of homologous and heterologous competition curves and analysis blocking and of "multiligand" dose-response surfaces (1990) Anal Biochem, 184, pp. 172-183
Sundberg, A. L., Blomquist, E., Carlsson, J., Cellular retention of radioactivity and increased radiation dose. Model experiments with EGF-dextran (2003) Nucl Med Biol, 30, pp. 303-315
Viney, J. L., Transgenic and gene knockout mice in cancer research (1995) Cancer Metastasis Rev, 14, pp. 77-90
Criteria for the design and biological characterization of radiolabeled peptide-based pharmaceuticals
Radiolabeled peptide-based formulations are being evaluated for their application in oncological imaging and therapy using nuclear medicine techniques. A major breakthrough in the field was the discovery and identification of the G-protein coupled receptor superfamily that are overexpressed in a variety of human cancers. These receptors act as targets for endogenous compounds, often of peptidic nature, which can be radiolabeled and, therefore, could potentially be utilized as radiopharmaceuticals. This general strategy has proven successful for application in humans in only a few cases thus far. However, the use of more sophisticated structural methodology to enhance our understanding of the interactions between the receptor and the endogenous peptide or its analogs, and a more efficient preclinical evaluation process, may help to single out the most promising compounds for further development and eventual use in the clinical application of radiopharmaceuticals. This review analyzes current methods of approaching these key points. The rational process for developing peptide-based radiopharmaceuticals is presented, from the structural analysis of the peptide-receptor interaction for the identification and modeling of the peptide analogs to the synthesis, with an appropriate metal carrier, of compounds that mimic endogenous peptides. Finally, the in vitro and in vivo biological testing and evaluation in preclinical animal models is described. To render the entire process successful, expertise in different areas of drug development is indispensable.
Criteria for the design and biological characterization of radiolabeled peptide-based pharmaceuticals
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